Bisaramil, an antiarrhythmic drug was developed as an inhibitor of calcium transport and as a membrane stabilizer. In addition, the drug showed tonic and frequency-dependent block that is most potent against the heart Na+ channel. However, the phase-II for Arrhythmias in Japan was discontinued.

Vidofludimus (SC12267; 4SC-101) is a novel oral immunomodulator inhibiting dihydroorotate dehydrogenase (DHODH) and the expression of proinflammatory cytokines including interleukin-17 (IL17A and IL17F) and interferon-gamma. This drug is in the clinical trial for the treatment of inflammatory bowel diseases and Rheumatoid arthritis.

Leteprinim is the synthetic purine. It has both anti-excitotoxic neuroprotective properties and enhances the regenerative response of surviving neurons within the central nervous system. Moreover, the experiments in vitro and in vivo reveal that leteprinim can be administered after an excitotoxic event and still produce neuroprotection. This is clearly crucial for any drug designed to treat stroke or any acute central nervous system injury. Therefore, leteprinim has the pharmacological properties required by a drug intended to treat acute stroke as well as a spinal injury. It may be useful in reducing brain injury; it possesses clinical relevance for the treatment of hypoxic-ischemic encephalopathy in the newborn. Leteprinim has the therapeutic potential for use in clinical trials in the treatment of neuronal deterioration in depression.

Deltibant is the bradykinin receptor antagonist. It was found to be a potent and selective inhibitor of the depressor response to bradykinin in the anaesthetized rat and rabbit. Deltibant affords significant protection against traumatic shock where bradykinin plays an important role in tissue injury. Such protection may be achieved through inhibition of neutrophil-endothelial interaction and protection of vascular endothelial function. Deltibant may have some effect on survival in patients with systemic inflammatory response syndrome and gram-negative sepsis. Kinin-kallikrein system could be involved in cerebral edema - treatment with deltibant appeared to alter the natural history of traumatic brain contusions by preventing the 2 degrees brain swelling. In addition, deltibant obviated the need for surgery in the majority of treated patients. Deltibant could act on the cerebral vasculature to limit dys-autoregulation and brain swelling or on the blood brain barrier to reduce cerebral edema. Deltibant has been in phase II clinical trials for the treatment of pain, immune-inflammatory diseases and stroke. However, this research has been discontinued.

Delmitide is the decapeptide with antiinflammatory activity. It is the first low molecular weight compound inhibiting TNF production at a translational level. Also, delmitide inhibits production of IFN-gamma, IL-12 and IL-2. It targets TRAF6/IRAK4/MyD88 complex and inhibits phosphorylation of SAPKs (p38 and JNK). Delmitide inhibits AP1 and NFkB activation. Delmitide was developed for the potential treatment of Crohn's disease and ulcerative colitis; phase II trials for both these indications commenced in October 2001. Phase I trial in chemotherapy-induced diarrhea and the gastrointestinal complications of HIV were also initiated. However, no recent development has been reported.